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Updated: Jul 16, 2026
10:17
Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Role of racemization in optically active drugs development
Imran Ali1, Vinod K Gupta, Hassan Y Aboul-Enein
1Department of Chemistry, Faculty of Natural Sciences, Jamia Millia Islamia University, Jamia Nagar, New Delhi, India.
Chirality
|March 30, 2007
Summary
Drug racemization, where optically active drugs convert into inactive forms in the body, poses safety risks. Understanding this process is crucial for determining safe drug dosages and marketing guidelines.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Drug Metabolism
Background:
- Optically active drugs can racemize in vivo, forming potentially toxic antipodes.
- Racemization reduces the effective concentration of the active drug enantiomer.
- Regulatory agencies like the U.S. Food and Drug Administration have guidelines for marketing such drugs.
Purpose of the Study:
- To describe the in vitro and in vivo racemization of optically active drugs.
- To investigate the influence of various factors on drug racemization.
- To propose safe dosage recommendations for optically active drugs.
Main Methods:
- Review of in vitro and in vivo studies on drug racemization.
- Analysis of racemization mechanisms.
- Discussion of factors affecting racemization kinetics (pH, temperature, concentration, ionic strength).
Main Results:
- Racemization is influenced by multiple variables including pH and temperature.
- Different optically active drugs exhibit varying racemization rates and mechanisms.
- Understanding these factors is key to predicting drug stability and efficacy.
Conclusions:
- Racemization of optically active drugs is a significant concern requiring careful study.
- Knowledge of racemization kinetics aids in establishing appropriate drug dosages.
- Further research into racemization mechanisms can improve drug safety and therapeutic outcomes.
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